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Assay Detail

CHEMBL4053933

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Functional
Antiproliferative activity against human Raji cells over expressing BTK after 48 hrs by CCK-8 assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Raji
Confidence 1 — Organism
Curated By Autocuration

Target

Raji (CHEMBL614628)
Type CELL-LINE
Organism Homo sapiens

Publication

Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia.
Liu H, Qu M, Xu L, Han X, Wang C, Shu X, Yao J, Liu K, Peng J, Li Y, Ma X.
Eur J Med Chem (2017) 135 : 60 -69
PubMed 28432946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.69 4.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086899 1 4.98
CHEMBL4065460 1 4.88
CHEMBL4094611 1 4.85
CHEMBL4061898 1 4.81
CHEMBL4103300 1 4.76
CHEMBL4097689 1 4.73
CHEMBL4092347 1 4.73
CHEMBL1873475 IBRUTINIB 4.0 1 4.71
CHEMBL4089960 1 4.65
CHEMBL3301625 SPEBRUTINIB 2.0 1 4.53
CHEMBL4074077 1 4.47
CHEMBL4070521 1 4.43
CHEMBL4071567 1 4.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086899 IC50 = 10500.0 nM 4.98
CHEMBL4065460 IC50 = 13200.0 nM 4.88
CHEMBL4094611 IC50 = 14200.0 nM 4.85
CHEMBL4061898 IC50 = 15500.0 nM 4.81
CHEMBL4103300 IC50 = 17400.0 nM 4.76
CHEMBL4097689 IC50 = 18700.0 nM 4.73
CHEMBL4092347 IC50 = 18700.0 nM 4.73
CHEMBL1873475 IBRUTINIB IC50 = 19300.0 nM 4.71
CHEMBL4089960 IC50 = 22400.0 nM 4.65
CHEMBL3301625 SPEBRUTINIB IC50 = 29400.0 nM 4.53
CHEMBL4074077 IC50 = 34100.0 nM 4.47
CHEMBL4070521 IC50 = 36900.0 nM 4.43
CHEMBL4071567 IC50 = 40900.0 nM 4.39